[~3H]-葫芦素B在动物体内的吸收、分布、排泄

口服~3H]-葫芦素B后,血药浓度变化属二室开放模型。各组织中放射性含量以肝、胆、胃、肺、肾及脾较高,脑组织最低,但连续给药后,小脑、胃、脑干放射性含量增加较为显著。小鼠灌药后24h尿液,未见原形药物。给药后96h,尿、粪排泄量分别占给药量的58.3％及35.8％,其胆汁中代谢物可经肠道再吸收。~3H]-葫芦素B的血浆蛋白结合率最大可达88.7％。

ABSORPTION,DISTRIBUTION,AND EXCRETION OF[~3H]-CUCURBITACIN B IN ANIMALS

After ~3H]-cucurbitacine B was administered to mice, the changein blood concentration of the drug accorded with the two compartment openmodel. The radioactivity levels in the liver, gallbladder, stomach, lung, kidneysand spleen, were higher, the lowest.was in the brain, but after repeated dosages,the radioactive levels increased obviously in cerebellum, stomach and brain stem.In the 24h urine no parent drug was detected. The total radioactivities excreted in 96h were 58.3% of the dose in urine and 35.8% in feces. Its metabolites frombile could be reabsorbed by intestine. The largest rate of drug binding withplasma protein could reach to 88.7%.